Peters Frank T, Meyer Markus R, Fritschi Giselher, Maurer Hans H
Department of Experimental and Clinical Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, University of Saarland, D-66421 Homburg (Saar), Germany.
J Chromatogr B Analyt Technol Biomed Life Sci. 2005 Sep 25;824(1-2):81-91. doi: 10.1016/j.jchromb.2005.07.003.
The aim of the presented study was to identify the metabolites of the new designer drug 4'-methyl-alpha-pyrrolidinobutyrophenone (MPBP) in rat urine using GC-MS techniques. After enzymatic hydrolysis, extraction and various derivatizations, seven metabolites of MPBP could be identified suggesting the following metabolic steps: oxidation of the 4'-methyl group to the corresponding alcohol and further oxidation to the respective carboxy compound, hydroxylation of the pyrrolidine ring followed by dehydrogenation to the corresponding lactam or reduction of the keto group to the 1-dihydro compound. A previously published GC-MS-based screening procedure for pyrrolidinophenones involving enzymatic hydrolysis and mixed-mode solid-phase extraction of urine samples allowed detection of MPBP metabolites. Assuming similar metabolism and dosages in humans, an intake of MPBP should be detectable via its metabolites in urine.
本研究的目的是使用气相色谱-质谱联用（GC-MS）技术鉴定新型设计药物4'-甲基-α-吡咯烷基丁苯酮（MPBP）在大鼠尿液中的代谢产物。经过酶解、提取和各种衍生化处理后，可鉴定出MPBP的七种代谢产物，提示以下代谢步骤：4'-甲基基团氧化为相应的醇，进一步氧化为相应的羧基化合物；吡咯烷环羟基化，随后脱氢为相应的内酰胺，或酮基还原为1-二氢化合物。先前发表的基于GC-MS的吡咯烷基苯酮筛查程序，包括尿液样本的酶解和混合模式固相萃取，可检测到MPBP的代谢产物。假设在人体内有相似的代谢和剂量，摄入MPBP后应可通过其尿液中的代谢产物检测到。
